非诺贝特固体自乳化制剂（S-SEDDS）体外评价及生物利用度研究

目的:以S-SEDDS替代液态自乳化制剂中的表面活性剂制备非诺贝特固体自乳化制剂。方法:比较了固体自乳化制剂与市售产品、液体自乳化制剂的体外溶出情况及体内生物利用度。结果:表明本研究的固体自乳化制剂用水分散后平均粒径为820.2±26.5(nm);溶出度试验结果显示,30min累积溶出度达到80%以上,本研究制备的非诺贝特固体自乳化制剂AUC(0-24)为22.7±8.2 mgoL-1oh与SEDDS的AUC(0-24)(24.9±7.6mgoL-1oh)没有显著性差异(P>0.05),与市售微粉化胶囊(13.8±10.5mgoL-1oh)相比能够显著提高药物的生物利用度(P<0.05)。结论:S-SEDDS有液体自乳化给药系统的效果。

The Solid Self-emulsified Drug Delivery System (S-SEDDS) of Fenofibrate:Evaluation in Vitro and Pharmacokinetic Studies in Vivo

Objective: The solid self-emulsified drug delivery system (S-SEDDS) of fenofibrate was investigated, which containedsolid excipient instead of surfactants usually used in liquid self-emulsified drug delivery system. Methods: Particle size distribution, dissolutionrate in vitro was detected. Rerults: The average size of S-SEDDS after dispersion was 820.2 ± 26.5 (nm). Dissolution test showedthat the accumulated dissolution of S-SEDDS was about 80% within 30min. In vivo study, AUC (0-24) was 22.7 ±8.2 mgoL-1oh inS-SEDDS and 24.9 ± 7.6 mgoL-1oh in SEDDS. There was no significant difference between S-SEDDS and SEDDS, while they were allbetter than that of the market capsule (13.8±10.5 mgoL-1oh). Conclusions: S-SEDDS could enhance the dissolution rate and the bioavailabilityof fenofibrate free of surfactant.